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Lomeguatrib | MGMT inhibitor

Lomeguatrib (192441-08-0) is a potent (IC50 = 9 nM) inhibitor of O6-Methylguanine-DNA Methyltransferase (MGMT), an important DNA repair protein.1 It is currently being investigated in cancers that have acquired resistant to the chemotherapeutic temozolomide2-5, as well as other chemotherapeutics6,7.

References/Citations
1) Reinhard et al. (2001), Monosaccharide-Linked Inhibitors of O6-Methylguanine-DNA Methyltransferase (MGMT): Synthesis, Molecular Modeling, and Structure-Activity Relationships; J. Med. Chem. 44 4050
2) Barvaux et al. (2004), Sensitization of a human ovarian cancer cell line to temozolomide by simultaneous attenuation of the Bcl-2 antiapoptotic protein and DNA repair by O6-alkylguanine-DNA alkyltransferase: Mol. Cancer Ther. 3 1215
3) Gumbrell et al. (2006), Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors: Clin. Cancer Res. 12 1577
4) Watson et al. (2009), O(6)-methylguanine-DNA methyltransferase depletion and DNA damage in patients with melanoma treated with temozolomide alone or with lomeguatrib: Br. J. Cancer 100 1250
5) Taspinar et al. (2013), Effect of lomeguatrib-temozolomide combination of MGMT promoter methylation and expression in primary glioblastoma tumor cells: Tumour Biol. 34 1935
6) Sabharwal et al. (2010), A phase I trial of lomeguatrib and irinotecan in metastatic colorectal cancer: Cancer Chemother. Pharmacol. 66 829
7) Tawbi et al. (2011), Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumors: Br. J. Cancer 105 773

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Catalog#  10-4017-0010

$50.00
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CAS:
192441-08-0
Catalog Number:
10-4017
Activity:
MGMT inhibitor
Chemical Name:
2-Amino-6-[(4-bromo-2-thienyl)methoxy]-9H-purine
Alternate Name:
O6-(4-Bromothenyl)guanine
Molecular Weight:
326.17
Molecular Formula:
C10H8BrN5O3S
Solubility:
Soluble in DMSO (up to 10 mg/ml with warming).
Physical Properties:
Off-white or beige solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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